State Key Laboratory of Natural Medicines and Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, PR China.
Eur J Med Chem. 2013 Oct;68:444-53. doi: 10.1016/j.ejmech.2013.07.041. Epub 2013 Aug 9.
A novel class of ocotillol-type triterpenoid derivatives have been synthesized and evaluated for their in vitro antibacterial activity against several representative pathogenic bacterial strains. Compounds 20(S)-protopanaxadiol (PPD), 3, 5, 16 and 24 exhibited potent antibacterial activity against Gram-positive bacteria. Compounds 3 and 5 also displayed promising antibacterial activity against a community-associated methicillin-resistant Staphylococcus aureus (CA-MRSA; strain USA300). Furthermore, compounds PPD, 3 and 16 combined with two commercially available antibiotics kanamycin and chloramphenicol showed strong synergistic inhibitory effects at their sub-MIC concentrations against S. aureus USA300 and Bacillus subtilis 168. Additionally, cytotoxic activity assay showed that the compounds tested did not affect cell viability of the human epithelial kidney (HEK-293) and human cervical (HeLa) cells at their MICs.
已经合成了一类新型的桉烷型三萜类衍生物，并评估了它们对几种代表性致病菌的体外抗菌活性。化合物 20(S)-原人参二醇（PPD）、3、5、16 和 24 对革兰氏阳性菌表现出很强的抗菌活性。化合物 3 和 5 对社区相关耐甲氧西林金黄色葡萄球菌（CA-MRSA；菌株 USA300）也显示出有希望的抗菌活性。此外，化合物 PPD、3 和 16 与两种市售抗生素卡那霉素和氯霉素在亚最低抑菌浓度下联合使用，对金黄色葡萄球菌 USA300 和枯草芽孢杆菌 168 表现出很强的协同抑制作用。此外，细胞毒性测定表明，在所测试的浓度下，这些化合物对人上皮肾（HEK-293）和人宫颈（HeLa）细胞的细胞活力没有影响。
